scholarly journals DESIGN, OPTIMIZATION, AND EVALUATION OF ACYCLOVIR FAST DISSOLVING TABLETS EMPLOYING STACH PHTHALATE – A NOVEL SUPERDISINTEGRANT

Author(s):  
SANTOSH KUMAR R ◽  
ANNU KUMARI

Objective: The objective of the present research was to prepare starch phthalate (a novel superdisintegrant) and to optimize and formulate acyclovir fast dissolving tablets employing 23 factorial design using starch phthalate as superdisintegrant. Materials and Methods: Drug excipient compatibility studies such as Fourier-transform infrared spectroscopy, differential scanning calorimetry, and thin-layer chromatography were carried out to check the drug interaction between acyclovir and starch phthalate. The direct compression method was used for tablet preparation. Prepared tablets were then evaluated for hardness, friability, drug content, disintegration time, water absorption, and wetting time, in vitro dissolution studies. Response surface plots and contour plots were also plotted to know the main effects and interaction effects of independent variables (starch phthalate [A], croscarmellose sodium [B], and crospovidone [C] on dependent variables [disintegration time and drug dissolution efficiency in 1 min]) and stability studies were also done. Results: Tablets of all formulations were of good quality concerning drug content (100±5%), hardness (3.6–4.0 kg/cm2), and friability (<0.16%). In all formulations, formulation F8 found to be optimized formulation with least disintegration time 9±3 s, less wetting time 10±0.17 s, and enhanced dissolution rate in 1 min, i.e., 99.92±0.11 as compared to other formulation. Conclusion: From the research, it was concluded that on combination with crospovidone (5%) and croscarmellose sodium (5%), starch phthalate (10%) enhanced the dissolution efficiency of the drug. Hence, starch phthalate can be used as a novel disintegrant in the manufacturing of fast dissolving tablets.

Author(s):  
R. SANTOSH KUMAR ◽  
KUMARI ANNU ◽  
B. KUSUMA LATHA ◽  
T. MALLIKA

Objective: The objective of the present research was to prepare starch phthalate (a novel super disintegrant) and to optimize and formulate ibuprofen fast dissolving tablets employing 23factorial design using starch phthalate as super disintegrant. Methods: Drug excipient compatibility studies like Fourier-transform infrared spectroscopy (FTIR) and thin-layer chromatography (TLC) studies were carried out to check the drug interaction between ibuprofen and starch phthalate. Direct compression method was used for tablet preparation. Prepared tablets were then evaluated for hardness, friability, drug content, disintegration time, water absorption and wetting time, in vitro dissolution studies. Response surface plots and contour plots were also plotted to know the main effects and interaction effects of independent variables (starch phthalate (A), croscarmellose sodium (B) and crospovidone (C)) on dependent variables (disintegration time and drug dissolution efficiency in 1 minute) and stability studies were also done. Results: Tablets of all formulations were of good quality concerning drug content (100±5%), hardness (3-6 kg/cm2), and friability (less than 0.16%). In all formulations, formulation F5 found to be optimized formulation with least disintegration time 20±0.28 seconds, less wetting time 09±0.12 seconds and enhanced dissolution rate in one minute, i.e., 91.95±0.22 as compared to other formulation. Conclusion: From the research, it was concluded that on combination with crospovidone, starch phthalate enhanced the dissolution efficiency of the drug. Hence, starch phthalate can be used as a novel disintegrant in the manufacturing of fast dissolving tablets.


2018 ◽  
Vol 10 (6) ◽  
pp. 249
Author(s):  
Santosh Kumar Rada ◽  
T. Naga

Objective: To synthesize, characterize and evaluate starch xanthate as a superdisintegrant in the formulation of fast dissolving tablets by employing 23 factorial design.Methods: Starch xanthate was synthesized by gelatinization process. The physical and micromeritic properties were performed to evaluate the synthesized starch xanthate. The fast dissolving tablet of ibuprofen was prepared by employing starch xanthate as a superdisintegrant in different proportions in each case by direct compression method using 23 factorial design. The drug content, hardness, friability, disintegration time and other dissolution characteristics like percent dissolved in 5 min (PD5), dissolution efficiency in 5 min (DE5%) and first order rate constant (K1) were used in the evaluation of prepared fast dissolving tablets.Results: The starch xanthate prepared was found to be fine, free flowing slightly crystalline powder. Starch xanthate exhibited good swelling in water. The study between ibuprofen and starch xanthate was shown the absence of interaction by fourier transform infrared spectra (FTIR) and differential scanning calorimetry (DSC). The drug content (100±5%), hardness (3.6–4 kg/sq. cm), and friability (0.12-0.15%) has been effective with regard to all the formulated fast dissolving tablets employing starch xanthate. The disintegration time of all the formulated tablets was found to be in the range of 12±0.01 to 312±0.02s. The optimized formulation F5 has the least disintegration time i.e., 12±0.01s. The In vitro wetting time of the formulated tablets was found to be in the range of 76±0.21 to 217±0.17s. The In vitro wetting time was less (i.e., 90s) in optimized formulation F5. The water absorption ratio of the formulated tablets was found to be in the range of 16±0.16 to 174±0.21%. The cumulative drug dissolved in the optimized formulation F5 was found to be 99.83±0.56% in 5 min.Conclusion: The dissolution efficiency of ibuprofen was enhanced when starch xanthate was found to be a superdisintegrant when combined with sodium starch glycolate, croscarmellose sodium and, hence it could be used in the formulation of fast dissolving tablets to provide immediate release of the contained drug within 5 min.


Author(s):  
Sudarshan Singh ◽  
S S Shyale ◽  
P Karade

The aim of this study was to design orally disintegrating tablet (ODT) of Lamotrigine. It is an Antiepileptic drug which is widely used in epilepsy. It is also used in simple and complex partial seizures and secondary generalized tonic-clonic seizures. It is poorly water soluble drug (0.46 mg/ml). Thus, an attempt was made to enhance the water solubility by complexation with β-cyclodextrin (1:1 molar ratios). The orally disintegrating tablet of lamotrigine was prepared by direct compression method using different concentration of superdisintegrants such as Sodium starch glycollate, croscarmellose sodium by sublimating agent such as camphor. The formulations were evaluated for weight variation, hardness, friability, drug content, wetting time, in vitro disintegration time and in vitro dissolution studies. The prepared tablets were characterized by Fourier transform infrared spectroscopy and differential scanning calorimetry. The disintegration time for the complexed tablets prepared by different concentration of superdisintegrants was found to be in range of 32.54 ± 0.50 to 55.12 ± 0.57 sec and wetting time of the formulations was found to be in range of 28.47 ± 0.67 to 52.19 ± 0.72 sec. All the formulation showed almost 100 percent of drug release within 15 min. Among all the formulation F6 and F7 prepared with 18% croscarmellose sodium and camphor shows faster drug release, respectively 10 min, F6 gives good result for disintegration time, drug release, wetting time and friability. Further formulations were subjected to stability testing for 30 days at temperature of 40 ± 5 ºC/75 ± 5 %RH. Tablets showed no appreciable changes with respect to physical appearance, drug content, disintegration time and dissolution profiles. Results were statistically analyzed by one-way ANOVA at a p < 0.05. It was found that, the data at any point of time are significant at p < 0.05.


2019 ◽  
Vol 9 (2) ◽  
pp. 160-169
Author(s):  
Rada Santosh Kumar ◽  
T. Naga Satya Yagnesh

The current scenario deals with the study of fast dissolving tablets for the patients suffering from swallowing, sickness ,etc.  The present investigation involves in the evaluation of starch tartrate as a superdintegrant in the formulation of fast dissolving tablets of poorly soluble drugs employing 23factorial design. Starch tartrate was synthesized by esterification process. The synthesized starch tartrate was subjected to physical and micromeritic evaluation. All fast dissolving tablets were evaluated for drug content, hardness, friability, disintegration time and other dissolution characteristics like percent dissolved in 5 min (PD5), dissolution efficiency in 5 min (DE5%) and first order rate constant(K1). The starch tartrate prepared was found to be fine, free flowing slightly crystalline powder. Starch tartrate exhibited good swelling in water.Fourier transform infrared spectra (FTIR) and Differential scanning calorimetry (DSC) study indicated the absence of interaction between ibuprofen and starch tartrate. All the fast dissolving tablets formulated employing starch tartrate were of good quality with regard to drug content (200±5%), hardness (3.6–3.9 kg/sq. cm), and friability (0.12-0.15%). The optimised formulation F2 has the least disintegration time i.e., 9±0. 03s. The in–vitro wetting time was less (i.e., 60s) in optimized formulation F2. The water absorption ratio of the formulated tablets was found to be in the range of 27.53±0.12 to 69.75±0.18%. The cumulative drug dissolved in the optimized formulation F2 was found to be 100.17±0.56% in 5 min. Starch tartrate was found to be a superdisintegrant which enhanced the dissolution efficiency with the ibuprofen and hence it could be used in the formulation of fast dissolving tablets to bring immediate release of the contained drug within 5 minutes. Keywords: Fast dissolving, Superdisintegrant, Starch tartrate, Dissolution efficiency.


Author(s):  
Santosh Kumar Rada ◽  
ANKITA GHOSH

Objective: To enhance the solubility of poorly soluble drugs by evaluating starch tartrate as a superdisintegrant in the formulation of fast dissolving tablets by employing 23 factorial design. Methods: Starch tartrate was synthesized by gelatinization process. The physical and micromeritic properties were performed to evaluate the synthesized starch tartrate. The fast dissolving tablets of piroxicam were prepared by using starch tartrate as a superdisintegrant in different proportions by direct compression technique using 23 factorial design. The drug content, hardness, friability, disintegration time and other dissolution characteristics like percent dissolved in 5 min (PD5), dissolution efficiency in 5 min (DE5%) and first-order rate constant (K1) were used in the evaluation of prepared fast dissolving tablets. Results: The superdisintegrant starch tartrate prepared was found to be fine, free-flowing slightly crystalline powder. Starch tartrate exhibited good swelling in water. The study between piroxicam and starch tartrate was shown the absence of interaction by fourier transform infrared spectra (FTIR) and differential scanning calorimetry (DSC). The drug content (99.83±0.56 %), hardness (3.7–3.9 kg/sq. Cm), and friability (0.12-0.15%) have been effective with regard to all the formulated fast dissolving tablets employing starch tartrate. The disintegration time of all the formulated fast dissolving tablets (FDTs) was found to be in the range of 12±0. 01 to 4500±0.02s. The optimized formulation F6 has the least disintegration time i.e., 12±0. 01s. The In vitro wetting time of the formulated tablets was found to be in the range of 35±0.09 to 1624±0.02s. The In–Vitro wetting time was less (i.e., 90s) in optimized formulation F6. The water absorption ratio of the formulated tablets was found to be in the range of 60±0.12 to 65±0.15%. The cumulative drug dissolved in the optimized formulation F6 was found to be 99.32±0.09% in 10 min. Conclusion: The dissolution efficiency of piroxicam was enhanced when starch tartrate was found to be a superdisintegrant when combined with crospovidone and, hence it could be used in the formulation of fast dissolving tablets to provide immediate release of the contained drug within 10 min.


2017 ◽  
Vol 9 (5) ◽  
pp. 51
Author(s):  
R. Santosh Kumar ◽  
T. Naga Satya Yagnesh ◽  
V. Goutham Kumar

Objective: To evaluate starch xanthate as a super disintegrant in the formulation of fast dissolving tablets of poorly soluble drugs employing 23 factorial design.Methods: Starch xanthate was synthesized by gelatinization process. The synthesized starch xanthate was subjected to physical and micromeritic evaluation. To establish as starch xanthate as a super disintegrant, fast dissolving tablet of ibuprofen was prepared employing starch xanthate in different proportions in each case by direct compression method employing 23 factorial design. All fast dissolving tablets prepared were evaluated for drug content, hardness, friability, disintegration time and other dissolution characteristics like percent dissolved in 5 min (PD5), Dissolution efficiency in 5 Min (DE5%) and first order rate constant(K1).Results: The starch xanthate prepared was found to be fine, free flowing slightly crystalline powder. Starch xanthate exhibited good swelling in water. Fourier transform infrared spectra (FTIR) and Differential scanning calorimetry (DSC) study indicated the absence of interaction between Ibuprofen and starch xanthate. All the fast dissolving tablets formulated employing starch xanthate were of good quality with regard to drug content(100±5%), hardness (3.6–4 kg/sq. cm), and friability (0.12-0.15%). The disintegration time of all the formulated tablets was found to be in the range of 13±0. 02 to 108±0.02s. The optimised formulation FL7 has the least disintegration time i.e., 13±0. 02s. The In vitro wetting time of the formulated tablets was found to be in the range of 90±0.15 to 369±0.17s. The In–Vitro wetting time was less (i.e., 90s) in optimized formulation FL7. The water absorption ratio of the formulated tablets was found to be in the range of 94±0.16 to 192±0.15%. The cumulative drug dissolved in the optimized formulation FL7 was found to be 99.63±0.24% in 5 min.Conclusion: Starch xanthate was found to be a super disintegrant which enhanced the dissolution efficiency when combined with sodium starch glycolate, croscarmellose sodium, with the ibuprofen and hence it could be used in the formulation of fast dissolving tablets to provide immediate release of the contained drug within 5 min.


Author(s):  
R. SANTOSH KUMAR ◽  
ANNU KUMARI ◽  
B. KUSUMA LATHA ◽  
PRUDHVI RAJ

Objective: The aim of the current research is optimization, preparation and evaluation of starch tartrate (novel super disintegrant) and preparation of fast dissolving oral films of cetirizine dihydrochloride by employing starch tartrate. Methods: To check the drug excipient compatibility studies of the selected drug (Cetrizine dihydrochloride) and the prepared excipient i. e starch tartrate, different studies like FTIR (Fourier-transform infrared spectroscopy), DSC (Differential scanning calorimetry) and thin-layer chromatography (TLC) were carried out to find out whether there is any interaction between cetirizine dihydrochloride and starch tartrate. The solvent casting method was used for the preparation of fast dissolving films. The prepared films were then evaluated for thickness, folding endurance, content uniformity, tensile strength, percent elongation, in vitro disintegration time and in-vitro dissolution studies. Response surface plots and contour plots were also plotted to know the individual and combined effect of starch tartrate (A), croscarmellose sodium (B) and crospovidone (C) on disintegration time and drug dissolution efficiency in 10 min (dependent variables). Results: Films of all the formulations are of good quality, smooth and elegant by appearance. Drug content (100±5%), thickness (0.059 mm to 0.061 mm), the weight of films varies from 51.33 to 58.06 mg, folding endurance (52 to 67 times), tensile strength (10.25 to 12.08 N/mm2). Fast dissolving films were found to disintegrate between 34 to 69 sec. Percent dissolved in 5 min were found to be more in F1 formulation which confirms that starch tartrate was effective at 1%. Conclusion: From the research conducted, it was proved that starch tartrate can be used in the formulation of fast dissolving films of cetirizine dihydrochloride. The disintegration time of the films was increased with increase in concentration of super disintegrant.


Author(s):  
R. SANTOSH KUMAR ◽  
SHAMBHAVI KANDUKURI ◽  
M. RAMYA ◽  
B. KUSUMA LATHA

Objective: To synthesize, characterize and evaluate starch valerate as a superdisintegrant in the formulation of aceclofenac fast dissolving tablets by employing 23 factorial design. Methods: Starch valerate was synthesized and its physical and micromeritic properties were performed to evaluate it. The fast dissolving tablet of aceclofenac was prepared by employing starch valerate as a superdisintegrant in different proportions in each case by direct compression method using 23 factorial design for evaluation of tablet parameters like disintegration and dissolution efficiency in 5 min. Results: The starch valerate prepared was found to be fine, amorphous and free flowing. Starch valerate exhibited good swelling in water with swelling index (125.2%). The study of starch valerate was shown by fourier transform infrared spectra (FTIR). The drug content (200±5%), hardness (3.5–4 kg/sq. cm), and friability (<0.15%) has been effective with regard to all the formulated fast dissolving tablets employing starch valerate. The disintegration time of all the formulated tablets was found to be in the range of 14±0.04 to 25.7±0.02 sec. The optimized formulation F4 had the least disintegration time i.e., 12.8±0.02 sec. The wetting time of the tablets was found to be in the range of 76±0.21 to 217±0.17s. The In vitro wetting time was less (i.e., 28±0.02s) in optimized formulation F4. The water absorption ratio of the formulated tablets was found to be in the range of 46±0.12 to 100±0.27%. The percent drug dissolved in the optimized formulation F8 was found to be 99.93% in 5 min. Conclusion: Starch valerate, when combined with sodium starch glycolate, croscarmellose sodium, with aceclofenac, was found to be an effective super disintegrant which improved the dissolution efficiency and could therefore be used in the formulation of quick dissolving tablets to provide immediate release of the contained drug within 5 min.


2015 ◽  
Vol 49 (3) ◽  
pp. 173-180
Author(s):  
T Ayyappan ◽  
C Poojitha ◽  
T Vetrichelvan

In the present work, orodissolving tablets of Efavirenz were prepared by direct compression method with a view to enhance patient compliance. A 23 full factorial design was applied to investigate the combined effect of three formulation variables. Amount of crospovidone, croscarmellose sodium and sodium starch glycolate were used as superdisintegrant material along with direct compressible mannitol to enhance mouth feel. The prepared batches of tablets were evaluated for hardness, friability, weight variation, disintegration time, wetting time, drug content and in-vitro dissolution studies. Based on wetting time, disintegration time, the formulation containing crospovidone (5% w/v), carscarmellose sodium (5% w/v) and sodium starch glycolate (8% w/v) was found to be promising and tested for in-vitro drug release pattern (in 0.1 N HCl), short term stability and drug- superdisintegrants interaction. Surface response plots are presented to graphically represent the effect of independent variables (conc. of superdisintegrants) on the in-vitro dissolution time. The validity of the generated mathematical model was tested by preparing extra-design check point formulation. The formulation showed nearly faster drug release compared to the conventional commercial tablet formulation. Stability studies on the optimized formulation indicated that there was no significant change found in physical appearance, hardness, disintegration time, drug content and in-vitro drug release. DOI: http://dx.doi.org/10.3329/bjsir.v49i3.22131 Bangladesh J. Sci. Ind. Res. 49(3), 173-180, 2014


Author(s):  
MEGHANA RAYKAR ◽  
MALARKODI VELRAJ

Objective: This study aims to Formulate Mouth Dissolving Tablets (MDTs) of Tofacitinib Citrate with the increase in bioavailability and patient compliance. Methods: Mouth Dissolving Tablets (MDTs) of Tofacitinib Citrate were developed by full factorial design at 32levelsand prepared by direct compression method using super integrants like sodium starch glycolate, Ludiflash. The tablets were compressed into compacts on a 10 station tablet machine. The bulk drug was characterised by determining, MP, Solubility, pH and FTIR spectra. Results: The weight variation, hardness and diameter, thickness, friability, drug content, wetting time, in vitro disintegration time and in vitro dissolution studies, and stability study, tablet thickness, weight variation and drug content post compression parameters remained consistent and reproducible. All the formulations showed, almost 100 percent of drug release within 75 min. Formulations F1, F2 and F3 were prepared with 5 mg of SSG and 20 mg, 30 mg, and 40 mg Ludiflash which shows % release of drug in the order of F1<F2<F3. Formulations F4, F5 and F6 were prepared with 10 mg of SSG and 20 mg, 30 mg, and 40 mg Ludiflash which shows % release of drug in the order of F4<F5<F6. Formulations F7, F8 and F9 were prepared with 15 mg of SSG and 20 mg, 30 mg, and 40 mg Ludiflash which shows % release of drug in the order of F7<F8<F9. Conclusion: It is concluded that the amount of superdisintegrants decreases disintegration time of tablets, decreases wetting time, increases the cumulative % drug release causes better absorption.


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